Gamma aminobutyric acid (GABA) agonists have been shown to have neuroprotective effects when used after focal or global cerebral ischemia. In this study, we evaluated the neuroprotective effects of a GABA re-uptake inhibitory agent, tiagabine, on focal ischemic brain injury in an embolic model in rats. Tiagabine, injected at 1 h after embolization, significantly reduced brain infarction volume, measured with 2,3,5-triphenyltetrazolium chloride (TTC) histological assay. There were varying degrees of neuroprotective effect exhibited in the other experimental groups however this did not reach significance. These results suggest that tiagabine is neuroprotective when administrated at an early period after the ischemic brain injury.